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Amphiphilic hyperbranched polyester coated rod mesoporous silica nanoparticles for pH-responsive doxorubicin delivery

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Rod-like mesoporous silica nanoparticles with pH-responsive amphiphilic hyperbranched polyester shells were prepared for doxorubicin (DOX) delivery. First, rod-shaped mesoporous silica nanoparticles (MSNs) were obtained, then hydrophobic hyperbranched polyester Boltorn H40 (H40) was grafted on their surface. The H40 coated MSNs were next treated with amine-functionalized polyethylene glycol (PEG) to achieve the hydrophilic and pH-responsive material denoted as PEG-H40-MSNs. The experimental results showed that PEG-H40-MSNs were successfully synthesized. BET analysis showed that rod MSNs exhibits a type IV standard isotherm. TEM revealed that the thin gray polymer layer was formed around the SBA-15 particle with a diameter of around 150 nm. DOX was effectively loaded, which can be released according to the ambient pH inside the cell as follow: at pH 7.4, only 9.7% of the DOX was released after 48 h; as the pH decreased to 5.5, the cumulative release reached to 49% at the same time. PEG-H40-MSNs showed less than 1.6% of hemolytic activity and a slight effect on the liver and kidney of treated mice were observed at a high disposal dosage implying negligible toxicities were caused by PEG-H40-MSNs in both in vitro hemolysis analysis and in vivo biochemical in mice. However, the in vitro cytotoxicity evaluation of the DOX-PEG-H40-MSNs showed that the cell cytotoxicity of both pure DOX and DOX-loaded PEG-H40-MSNs generally enhanced by increasing the concentration of DOX.

Schematic of cellular uptake and DOX release of PEG-H40-MSNs nanoparticle

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This work was financially supported by the Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

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Correspondence to Rassoul Dinarvand.

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Bafkary, R., Ahmadi, S., Fayazi, F. et al. Amphiphilic hyperbranched polyester coated rod mesoporous silica nanoparticles for pH-responsive doxorubicin delivery. DARU J Pharm Sci (2020). https://doi.org/10.1007/s40199-020-00328-x

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  • Mesoporous silica nanoparticles
  • Hyperbranched polyester
  • pH-responsive drug delivery